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Drugs. 2020 Apr;80(5):513-521. doi: 10.1007/s40265-020-01288-x.
Tazemetostat (Tazverik™), a first-in-class, small molecule enhancer of zeste homolog 2 (EZH2) inhibitor, received accelerated approval in January 2020 in the USA for the treatment of adults and adolescents aged ≥ 16 years with locally advanced or metastatic epithelioid sarcoma not eligible for complete resection. Developed by Epizyme, in collaboration with Eisai, it is the first therapy to be approved specifically for the treatment of epithelioid sarcoma in the USA. The recommended dosage regimen is 800 mg twice daily, administered orally with or without food, until disease progression or unacceptable toxicity. Tazemetostat is also undergoing clinical development in various countries worldwide for use in several other tumour types, including diffuse large B-cell lymphoma and mesothelioma, with the US FDA accepting a New Drug Application and granting priority review for its use in the treatment of follicular lymphoma. This article summarizes the milestones in the development of tazemetostat leading to this first approval for the treatment of adults and adolescents aged ≥ 16 years with locally advanced or metastatic epithelioid sarcoma not eligible for complete resection.
他泽司他（Tazverik™）是一种首创的、小分子增强子结合蛋白 2（EZH2）抑制剂，于 2020 年 1 月在美国获得加速批准，用于治疗不符合完全切除条件的局部晚期或转移性上皮样肉瘤的成人和青少年（≥ 16 岁）。该药由 Epizyme 与 Eisai 合作开发，是美国首个专门获批用于治疗上皮样肉瘤的疗法。推荐剂量方案为 800mg，每日两次，口服，可与食物同服或不同服，直至疾病进展或出现不可接受的毒性。他泽司他还在全球多个国家进行临床开发，用于治疗其他几种肿瘤类型，包括弥漫性大 B 细胞淋巴瘤和间皮瘤，美国 FDA 已接受该药用于治疗滤泡性淋巴瘤的新药申请，并给予优先审评。本文总结了他泽司他开发过程中的重要里程碑，从而首次获得批准用于治疗不符合完全切除条件的局部晚期或转移性上皮样肉瘤的成人和青少年（≥ 16 岁）。
